Effervescent mouthwash tablet

ABSTRACT

AN EFFERVESCENT MOUTHWASH TABLE COMPRISING AN EFFERVESCENT COUPLE, AND AN ASTRINGENT-DESENSITIZING AGENT. FLAVORING, COLOR, SWEETENER AND OTHER ADDITIVES MAY BE ADDED TO THE BASIC FORMULA. UPON DISSOLUTION A SOLUTION IS PRODUCED WHICH GIVES A CLEANSING MOUTHWASH EFFECT, EFFECTIVE DOSENSITIZING ACTION TO THE TEETH, AND GINGIVAL TONING. THIS SOLUTION FORMS A DESIRABLE AND UNIQUE BASIS FOR THE ADDITION OF FURTHER AGENTS WHICH WILL AID IN CONTROL OF PLAQUE, BREATH SWEETENING, ANTI-MICROBIAL EFFECT, DECAY PREVENTION, WATER PURIFICATION, AND LONG LASTING EFFECT OF ALL ABOVE MENTIONED.

United States Patent m 3,772,431 EFFERVESCENT MOUTHWASH TABLET WilliamP. Mlkvy, Hollystone Farm, RD. 2, Holland, Pa. 18966, and Raymond J.Tucci, 347 Saly Road, Yardley, Pa. 19067 No Drawing. Filed Sept. 21,1972, Ser. No. 290,914 Int. Cl. A61k 9/00, 11/02, 11/04 US. Cl. 424-44 4Claims ABSTRACT OF THE DISCLOSURE An effervescent mouthwash tabletcomprising an effervescent 'couple, and an astringent-desensitizingagent. Flavoring, color, sweetener and other additives may be added tothe basic formula.

Upon dissolution a solution is produced which gives a cleansingmouthwash effect, effective desensitizing action to the teeth, andgingival toning. This solution forms a desirable and unique basis forthe addition of further agents which will aid in control of plaque,breath sweetening, anti-microbial effect, decay prevention, waterpurification, and long lasting effect of all above mentioned.

This invention relates to an effervescent tablet which when dissolved inwater produces a solution which makes it uniquely desirable for use as amouthwash.

The use of mouthwashes in liquid form is Well known and popular.However, for many years, the appropriation of a mouthwash from a drypowder had has appeal because it is freshly made instead of having beencontained in a bottle for a long period of time. The application of thisprinciple to an effervescent formula has surprisingly attracted littleattention, although offering advantages of freshness, taste andeffectiveness, as will be set forth hereinafter.

Furthermore, it has been difficult for a traveler, such as a tourist ora camper, to carry liquid mouthwash with him because of weight,fragility or bulk. Furthermore, shelf space is a problem at the retailoutlet or even the home and so the provision of a number of tablets iseasily preferable to a pint of liquid or the bulky sizes greater than apint.

Also, a tablet being of powder is not subject to atmospheric changes ortemperature changes and would be convenient for use by the airlines oron a ship. The tablet would be useful even where the quality of drinkingwater is a problem since the formula can be modified to include a waterpurification chemical.

Effervescent tablets for producing cleaning compositions have beenfonmulated in the past.

The concept of an effervescent tablet has been previously recognized inUS. Pats. Nos. 1,450,865, 2,105,- 690, 2,540,253, 2,985,562, 2,999,293,3,102,075, 3,105,- 792, 3,136,692 and 3,653,914. Also to be consideredis Pat. No. 3,518,343 which introduces an anti-microbial substance intothe effervescent tablet as well as a special tablet lubricant. -Itshould be noted, however, that each of the prior arts has had as itsprimary purpose avoidance of technical difficulties associated with theproduction and tableting of the effervescent tablet. The primaryconsideration was not for the development of a useful andacceptablemouthwash tablet, but of a producable effervescent tablet withmouthwash application. The formulas in each instance produce a sweet,pleasant-tasting, colored mixture, not unlike a soda drink.

Heretofore, astringent-desensitizing agents have been regarded asunacceptable because of their apparent insolubility in the presence of acarbonate or bicarbonate. These agents will be later outlined with thesolution as presented by the present invention. The lack of said agentsin previous effervescent mouthwash tablet formulations is most likelyresponsible to some degree for the noted absence 3,772,431 Patented Nov.13, 1973 of a commercially acceptable and practically usefuleffervescent mouthwash tablet. It is our purpose to produce aneffervescent mouthwash tablet which will be not only palatable inappearance and taste, but which will have the dual role of producing anastringent mouthwash effect and desensitizing action, and which formwill lend itself ideally and uniquely to the additions as outlined inour claims for long lasting plaque control, decay control,anti-microbial action, breath sweetening whitening, and waterpurification.

Without this basic and necessary astringent-desensitizer, the tabletwith all additives will be unappealing and therefore non-useful.

The effervescent granulation can be selected from formulations wellknown to those skilled in the art. The composition consists of at leastone each of a solid acid and solid basic material which react to produceCO when dissolved in water, causing the effervescence. The acid may bean organic such as fumaric, citric, tartaric, etc., or a correspondinganhydride or an inorganic, such as sulfamic or phosphonic acidderivative as disclosed in Pat. No. 3,325,357. The basic material can beany of the metal carbonate salts such as alkali or alkaline earthcarbonates and bicarbonates. Lithium, sodium, calcium carbonates orbicarbonates are examples of such materials. Certain combinations of theacids and bases are preferable to others. In the present invention, thetablet is prepared as follows:

(I) Basic effervescent granules: Parts by weight Tartaric acid andsodium bicarbonate are passed through 40 mesh screen, neither arepre-heated as is usually directed. Materials blended and heated on awater bath in a porcelain evaporating dish. Mixture is stirred as itbecomes moist with glass or stainless steel device (Temperature about C.under dish). Screen through 8 mesh screen and heat to two hours in ovenat 40 C. When damp granules are dry, push through 16 mesh screen andstore over silica gel or equivalent desiccant.

The astringent-desensitizing agent may be:

( 1) Tannic acid and the tanin group.

(2) Dilute or weak salts of the metals such as zinc chloride, stannicchloride, strontium chloride, alums, aluminum chloride and acetate.

(3) Dilute organic acids such as basic acid.

Examples of the foregoing are:

(1) Zinc chloride 2) Strontium chloride (3) Thymol (4) Silver nitrate(5) Sodium carbonate (anhydrous) (6) Trichloroacetic acid (7) Procainehydrochloride (8) Potassium hydroxide (9) Phenol (10) Oil of clove (llEugenol (12) Crissote (13) Chlorobutanol 14) Ammoniacal silver nitrateThe use of strontium chloride in aqueous solution has presenteddifficulties in the past because the strontium chloride has a very lowsolubility product in prescence of carbonate and bicarbonate. Theresulting precipitation would be undesirable because the insolubleprecipitate would undoubtedly be available to function as anastringent-desensitizing agent and there would be further objection froman appearance standpoint.

With the present invention, it is now possible to maintain the strontiumchloride in aqueous solution at a 2 to 15% by weight concentrationthrough the use of effervescent granulation Formula .#1 that maintains asolution The invention contemplates additional active ingredients, butthis is by way of the more specific aspects of the invention. Theinvention as previously described in itself constitutes an effectivemouthwash tablet, but the pH of about 5 during the course of carbondioxide gener- 5 ingredients to be discussed hereinafter contributeother ation. Furthermore, the tablet will dissolve in Water in desirableproperties and so will be incorporated many twenty to thirty seconds toproduce a clear aqueous solutimes in the basic formula. These additionalingredients tion that has effective astringent and desensitizingpropinclude an anti-microbial agent, an adherent, a chelating erties.agent and vitamin C as well as the usual tablet lubricants.

A common dental problem is that of extra sensitive m The preferredanti-microbial agent is cetyldimethylteeth. When the dentin or cementumof the tooth is exbenzylammonium chloride. Many anti-microbial agentsposed because of faulty brushing, abrasion, gum diseases, may be used,including phenol and its homologs and etc., then cold, heat, sour,sweet, or pressure contacts derivatives such as alkyl phenols,halogenated phenols, these areas and causes discomfort. In aqueoussolution polyhydric phenols and a diphenyl and similar aryl derivathestrontium ion is released. This ion appears to have tives. Otheranti-microbial substances are set forth in a strong adsorptive affinityfor the organic fraction of US. Pat. No. 3,518,343 and such substances,as specificalcified tissue (dentin and cementum). The higher the callymentioned in columns 4 and 5 of said patent, and organic content thegreater the absorption. The strontium elsewhere throughout said patent,are expressly incorpoion was shown to be effective in relievingsensitivity by rated herein by reference. virtue of its apparentbiocolloidal binding and blocking However, with the present invention ithas been disactions. The ions penetrate into the dentinal tubules incovered that the use of anti-microbial agent is not enough depth. Thisis consistent with the hypothesis that as the to launch an effectiveattack into tooth decay and the strontium ion binds with thebiocolloidals of the organic mechanism which causes tooth decay. matrix,an effective blockade is established to disrupt the r A prime cause oftooth decay is believed to occur with transmission of external stimulito the dental pulp. the formation of mucin which is an albuninoidsubstance Formula A1 Formula A; Formula B Grams Grams Percent GramsPercent Effervescent granulation 1. 20 1.20 61.95 1.20 58.97 Granularmannitol 0. 400 0. 400 20. 65 0. 300 14. 74 Green color 0.002 0. 002 0.10 Ascorbic acid 0. 100 0.100 5.16 0. 100 4. 91 trontium chloride. 0.040 0. 100 5. l6 0. 300 14. 74 Sodium saccharim. 0.020 0.020 1. 03 0.020 0. 98 Sodium benzoate 0. 015 0.015 0. 77 0. 015 0. 74 Peppermint dryflavo 0.100 0. 100 5.16 0. 100 4. 91

Total 1. 877 1. 937 99. 9s 2. 035 99. 99

Another astringent and desensitizing agent is zinc chlofound in themouth. Mucin acts as a binding material to ride. This is especiallydesirable for its astringent effect, hold bacteria, calcium and fooddebris together in a mass giving good gingival toning and very goodfeeling to the 40 that is collectively referred to as plaque. Mucin isinsoluble mouth after use. It also is an effective desensitizer. Howinwater, but is precipitated by vitamin C. With the preever, its action,rather than one of binding and blocking cipitation of mucin, inconjunction with the present inwith the strontium ion released from thestrontium chlovention, a synergistic effect is achieved by virtue of theride, is an action of cauterization of the exposed dentinalanti-microbial agent and the chelating agent of the present tubules. Itthereby establishes an effective blockade, disinvention. rupting thetransmission of external stimuli to the dental The present inventioncontemplates the action of vitapulp. Zinc chloride may be used as thesole astringentmin C, which when present in sufiicient quantities, willdesensitizer or may be used in conjunction with the stroncut the mucinand this will have a significant effect in tium chloride, enhancing theeffect of each. When used in minimizing the amount of mucin that remainsactive to conjunction with each other, it shall be called an astrinre Pq The ehelaiihg agent Will hold calcium s gent-desensitizer system. Inthe event that it becomes in solution and retard the depo i i n of Calcum ions in difficult to work with zinc chloride, then ammonium alutheremaining plaque, as allowed by the minimal amount minium sulfate andpotassium aluminum sulfate may be of mucin. Finally, the anti-microbialagent will deprive utilized as alternative astringents. Whatever plaqueis formed of any significant bacteria The active astringent anddesensitizing agent may be vahle, thus further deactivating the P q andtending any one of those mentioned above or may be a combinato defeatthe formation of calculus which leads to tooth tion where one has acauterizing effect, and the other a ecay. binding effect; one enhancingthe other. In addition, the bubbling effect produced by the effer-Desensitizing agents have been used in toothpaste form, vescentgranulation formula has a value in removal of The value of these agentsin an effervescent mouthwash plaque debris, and also stimulates theblood circulation form is evident. The act of brushing and the pasteitself of the Oral a. act as abrasives. Amouthwash is gentle,non-abrasive, and Yet another important substance o e added in the ineffervescent tablet form has the added advantage of actual Preparationof the pl'eselIt invention is the use Of being easily used in situationswhere toothbrushing and all adherent, such as sodium behzoate, beIlZOiei r carrying of a liquid mouthwash would be impractical. P Y WSR301, aresihe'hs adherent The Presence of This is an important consideration asthe effect of h the adherent enables the entire formula to have longdesensitizer is cumulative. In actual preparation of the lasting P P Theadherent is a Water Soluble agent effervescent mouthwash tablet it wouldbe important to that acts as a Vehicle for the active components of theincorporate certain other substances which would greatly formula, Withthe adherent in its adhering eifechvehess add to the value of the tabletto the consumer. However tending to form a film 011 the teeth that isnot readily it is felt that without the basis of the present invention slu l in water or saliva- Thus. such a film Will Persist as stated, theseadditional substances would not be acfor a Considerable time, therebyholding the active ceptable in effervescent mouthwash tablet form.gredients in continuing contact with the teeth. This further In actualpreparation, consideration has been given to aids in the destruction ofmucin and the prevention of the use of an anti-microbial agent.formation of plaque.

A chelating agent will sequester calcium in solution,

.vvithout any damage to enamel, and permit it to be washed Anothermouthwash tablet utilizing zinc chloride has the following formulation:

away with the effervescent formulation, thereby prevent- Lower, g. ing'continuing build-up of dental plaque, the primary Effervescentgranulation 1.200 cause of tooth decay. Preferred chelating agents are 5Granular mannitol 0.400 EDTA. disodium dihydrogenethylenediaminetetraacetate Turquois Green 0.002 and'the calcium chelateof disodium ethylenediaminetetra- Ascorbic acid 0.100 acetic acid. Zincchloride 0.150 Finally, it may be aesthetically desirable to add anSodium saccharin 0.020 optical whitener to the basic formula. Also, afluoride and 10 Sodium benzoate 0.015 a water purification chemical canbe added. Peppermint dry flavor 0.100

It is felt that these particular additives made practical through theuse of the present invention, will be of inesti- The use Of Sweetenersand flavoring agents is Well bl value i th t f preventive dentistry Whknown to those skilled in the art and the relative amounts the dentisthas always encouraged people to at least rinse y be adjusted to faste-Sodium saeeharinmay b used the mouth with Water, if brushing is notpossible after p to one Pereeht y Weight Flavoring agents, Such as foodconsumption, a palatable, astringent-effervescent peppermint andcinnamon, may be used in amounts by mouthwash tablet makes this nowpossible and practical, weight ranging from 0.2 to 5 percent by weight.with the added health benefits as stated. The adherent is preferablypresent in an amount by The other components of the various formulae ofsaid weight ranging from 0.25 to 4%. 3,513,343 are e lncelpofated herelhy Vitamin C is preferably present in an amount by weight erence to theextent consistent with the present invention, ranging f 1 to mffludmgthe tablettmg and oiher manufacturing tech The chelating agent ispreferably present in an amount 2:35: iz i gz the the tablet and the byweight ranging from 0.001% to 0.010%. The foregoing as well as otherobjects of the inven- 25 The z i gz is preferably present In an tion areachieved by providing a balanced formula of an 9; n y 5. .rangmg i toeffervescent mouthwash tablet that can be readily formue desensitlzmgagent is Preferably present In an lated and compressed into tablet formby well known amountbywelghtrangmgfwm1t15%- machinery. The product isbelieved to possess along shelf The efiervf'scent agent 15 PreferablyPresent In an life and will consistently provide an aqueous solution ofamouflt by Welght rangmg from 40% to good 1 and taste as l as l i It 18also contemplated that a fluorescent whitener be 1 A mouthwash withplaque control agent has the foladded to the overall formula in anamount not to exceed lowing formulation: one percent by weight.

FORMULA N0. 1

Per tablet Lower, g. Grams Percent Upper, g.

Effervescent granulation (N0. 2) 1. 200 59.14 Mannitol granular (20 meshtabletting agen 0. 200 0. 400 Ascorbic acid (Vitanun C) 0.050 0. Zinechloride (desensitizing) 0. 050 0. 150 Sodium saccharin 0. 005 0. 010Sodium benzoate (100 mesh adherent) 0. 005 0. 015 V'erdent Green MX 0.004 Peppermint dry flavor- 0.

Total Another formula for use in the present invention possesses thefollowing constituent elements:

Total Per tablet Lower, g. Grams Percent Upper, g.

Effervescent granulation (N0. 2) 1. 200 Mannitol granular (20 mesh). 0.200 0. 400 Ascorbic acid (Vitamin 0).-.. .050 0.100Cetyldimethylbenzylammom'um chloride. 0 010 0. 040 Sodium saccharin 0.005 0. 010 Polyox WS R-301 (resinous adherent) 0. 010 0. 030

'Versene CA (calcium disodium EDTA) 0.0001 Verdent Green MX 135 0. 004Peppermint dry flavor 0.150

A mouthwash tablet with resinous adherent for long lasting flavor hasthe following formulation:

The present invention further contemplates the inclusion of vitamin B.

We claim:

1. An effervescent mouthwash tablet comprising an effervescent coupleconsisting of at least one each of a 5 solid pharmaceutically acceptableacid and a solid pharmaceutically acceptable base material, whicheffervescent couple reacts to produce carbon dioxide when dissolved inwater causing elfervescence, and an effective amount of strontiumchloride, zinc chloride and mixtures thereof as anastringent-desensitizing agent.

2. The tablet of claim 1 wherein said astringent and desensitizing agentis strontium chloride.

3. The tablet of claim 1 wherein said astringent and desensitizing agentis zinc chloride.

4. An effervescent reaction product produced when the tablet of claim 1is dissolved in water, said product having a pH of about 5.

References Cited UNITED STATES PATENTS 3,518,343 6/1970 Welsh et a1.424--44 3,629,468 12/ 1971 Andersen 424-44 OTHER REFERENCES Brown, H.K., J. Can. Dental Assoc. 16: 523-6 (1950), Status of Dental CariesPreventive Measures in 1950.1

SHEP K. ROSE, Primary Examiner U.S. Cl. X.R. 424-49

